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AR128043A1 - SALTS AND SOLID FORMS OF AN FGFR INHIBITOR AND PROCESSES FOR THEIR PREPARATION - Google Patents

SALTS AND SOLID FORMS OF AN FGFR INHIBITOR AND PROCESSES FOR THEIR PREPARATION

Info

Publication number
AR128043A1
AR128043A1 ARP220103523A ARP220103523A AR128043A1 AR 128043 A1 AR128043 A1 AR 128043A1 AR P220103523 A ARP220103523 A AR P220103523A AR P220103523 A ARP220103523 A AR P220103523A AR 128043 A1 AR128043 A1 AR 128043A1
Authority
AR
Argentina
Prior art keywords
acid
salt
formula
salts
solid form
Prior art date
Application number
ARP220103523A
Other languages
Spanish (es)
Inventor
Pingli Liu
Zhongjiang Jia
Qiyan Lin
Naijing Su
Timothy Martin
Michael Xia
Jiacheng Zhou
Baoyu Mi
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of AR128043A1 publication Critical patent/AR128043A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se refiere a sales y formas sólidas del inhibidor de FGFR (7R,8aS)-2-(5-(5-(2,3-dimetilfenil)-6-metoxi-1H-pirazolo[4,3-b]piridin-3-il)piridin-2-il)octahidropirrolo[1,2-a]pirazin-7-ol, e incluye métodos para su preparación, en donde los compuestos, las sales y las formas sólidas son útiles en el tratamiento de enfermedades mediadas por FGFR, tales como el cáncer. Reivindicación 1: Una forma sólida del Compuesto 1 con la fórmula: (1), caracterizada porque la forma sólida es cristalina. Reivindicación 17: Una sal caracterizada porque es una sal de adición de ácido del Compuesto 1, que tiene la estructura: de fórmula (1), en donde el ácido es ácido fosfórico, ácido clorhídrico, ácido L-tartárico, ácido malónico, ácido metanosulfónico, ácido adípico, ácido fumárico, ácido maleico, ácido málico o ácido succínico. Reivindicación 82: Un proceso para preparar el Compuesto 1 con la fórmula: (1), o una sal de este, caracterizado porque comprende: desproteger el Compuesto 2 con la fórmula: (2), o una sal de este, con A1, en donde A1 es un ácido. Reivindicación 117: Una composición farmacéutica caracterizada porque comprende una forma sólida de cualquiera de las reivindicaciones 1 - 16, o una sal de cualquiera de las reivindicaciones 17 - 81, y un portador o excipiente farmacéuticamente aceptable. Reivindicación 118: Un método para inhibir una enzima FGFR3, caracterizado porque comprende poner en contacto una forma sólida de cualquiera de las reivindicaciones 1 - 16 o una sal de cualquiera de las reivindicaciones 17 - 81 con dicha enzima.The present invention relates to salts and solid forms of the FGFR inhibitor (7R,8aS)-2-(5-(5-(2,3-dimethylphenyl)-6-methoxy-1H-pyrazolo[4,3-b] pyridin-3-yl)pyridin-2-yl)octahydropyrrolo[1,2-a]pyrazin-7-ol, and includes methods for its preparation, where the compounds, salts and solid forms are useful in the treatment of FGFR-mediated diseases, such as cancer. Claim 1: A solid form of Compound 1 with the formula: (1), characterized in that the solid form is crystalline. Claim 17: A salt characterized in that it is an acid addition salt of Compound 1, having the structure: of formula (1), wherein the acid is phosphoric acid, hydrochloric acid, L-tartaric acid, malonic acid, methanesulfonic acid , adipic acid, fumaric acid, maleic acid, malic acid or succinic acid. Claim 82: A process for preparing Compound 1 with the formula: (1), or a salt thereof, characterized in that it comprises: deprotecting Compound 2 with the formula: (2), or a salt thereof, with A1, in where A1 is an acid. Claim 117: A pharmaceutical composition characterized in that it comprises a solid form of any of claims 1 - 16, or a salt of any of claims 17 - 81, and a pharmaceutically acceptable carrier or excipient. Claim 118: A method for inhibiting an FGFR3 enzyme, characterized in that it comprises contacting a solid form of any of claims 1-16 or a salt of any of claims 17-81 with said enzyme.

ARP220103523A 2021-12-22 2022-12-21 SALTS AND SOLID FORMS OF AN FGFR INHIBITOR AND PROCESSES FOR THEIR PREPARATION AR128043A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202163292628P 2021-12-22 2021-12-22

Publications (1)

Publication Number Publication Date
AR128043A1 true AR128043A1 (en) 2024-03-20

Family

ID=85172903

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP220103523A AR128043A1 (en) 2021-12-22 2022-12-21 SALTS AND SOLID FORMS OF AN FGFR INHIBITOR AND PROCESSES FOR THEIR PREPARATION

Country Status (16)

Country Link
US (1) US20230192722A1 (en)
EP (1) EP4452982A1 (en)
JP (1) JP2025500466A (en)
KR (1) KR20240136984A (en)
CN (1) CN118660889A (en)
AR (1) AR128043A1 (en)
AU (1) AU2022418585A1 (en)
CA (1) CA3244187A1 (en)
CL (1) CL2024001873A1 (en)
CO (1) CO2024009568A2 (en)
CR (1) CR20240297A (en)
IL (1) IL313735A (en)
MX (1) MX2024007951A (en)
PE (1) PE20250776A1 (en)
TW (1) TW202340215A (en)
WO (1) WO2023122134A1 (en)

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CR20230467A (en) 2021-03-10 2024-02-20 Jnana Therapeutics Inc SMALL MOLECULE INHIBITORS OF MAMMALIAN SLC6A19 FUNCTION
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

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Also Published As

Publication number Publication date
CN118660889A (en) 2024-09-17
CR20240297A (en) 2024-09-18
JP2025500466A (en) 2025-01-09
AU2022418585A1 (en) 2024-07-11
PE20250776A1 (en) 2025-03-14
CO2024009568A2 (en) 2024-07-29
TW202340215A (en) 2023-10-16
IL313735A (en) 2024-08-01
CA3244187A1 (en) 2023-06-29
WO2023122134A1 (en) 2023-06-29
US20230192722A1 (en) 2023-06-22
MX2024007951A (en) 2024-07-10
EP4452982A1 (en) 2024-10-30
KR20240136984A (en) 2024-09-19
CL2024001873A1 (en) 2024-12-06

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